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CAS No. : 2247127-79-1
MCE 国际站:Glutaminase-IN-1
产品活性:Glutaminase-IN-1 (CB839 derivative) 是CB839 的一个衍生物,是1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂,其IC50 值为1 nM。Glutaminase-IN-1 (CB839 derivative) 具有提高细胞摄取和抗肿瘤的活性。
研究领域:Metabolic Enzyme/Protease
作用靶点:Glutaminase
In Vitro: Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC50 values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839.
In Vivo: Glutaminase-IN-1(10 mg/kg, s.c.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing mice.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Glutamine Metabolism Compound Library | Anti-Cancer Metabolism Compound Library | Mitochondria-Targeted Compound Library | Cuproptosis Compound Library | Heterocyclic Compound Library | ZED-1227 | Glutaminase-IN-4 | GLS1 Inhibitor-4 | Zampilimab | NC9 | Cystamine-d8 (dihydrochloride) | BJJF078 | GLS1 Inhibitor-6 | Telaglenastat | Cystamine | LWG-301 | Glutaminase C-IN-1 | IPN60090 | GK921 | JHU-083 | A-446 | 2-Amino-2-(p-tolyl)acetic acid | 6-Diazo-5-oxo-L-nor-Leucine | L-Albizziin | BPTES | GLS-1-IN-1 | NTU281 | TG-2-IN-1 | α-Glucosidase-IN-5 | UPGL00004 | GLS1 Inhibitor-3 | Glutaminase-IN-3
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
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货号: HY-114334
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